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Description: Selective inhibitor of Akt/PKB signaling. Antitumor and antiviral
Alternative Names: Triciribine,NSC 154020,TCN
Chemical Name: 1,5-Dihydro-5-methyl-1-β-D-ribofuranosyl-1,4,5,6,8-pentaazaacenaphthylen-3-amine
Purity: ≥99% (HPLC)
Biological Activity for API-2
API-2 is a selective inhibitor of Akt (protein kinase B) signaling; displays minimal inhibition of PKC, PKA, SGK and p38 pathways. Inhibits phosphorylation and activation of downstream targets of Akt including Bad, GSK-3β and AFX. Induces apoptosis and growth arrest in vitro, preferentially in human cancer cells with elevated levels of Akt. Potently and selectively inhibits growth of Akt-overexpressing tumors in mice. Inhibits DNA synthesis and displays antiviral activity against HIV-1 and -2.
Compound Libraries for API-2
API-2 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.
Technical Data for API-2
| M. Wt | 320.31 |
| Formula | C13H16N6O4 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 35943-35-2 |
| PubChem ID | 65399 |
| InChI Key | HOGVTUZUJGHKPL-HTVVRFAVSA-N |
| Smiles | O[C@@H]1[C@@H](CO)O[C@@H](N2C3=C(C4=NC=N3)C(C(N)=NN4C)=C2)[C@@H]1O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for API-2
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 1eq. HCl | 32.03 | 100 | |
| DMSO | 32.03 | 100 |
Preparing Stock Solutions for API-2
The following data is based on the product molecular weight 320.31. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.12 mL | 15.61 mL | 31.22 mL |
| 5 mM | 0.62 mL | 3.12 mL | 6.24 mL |
| 10 mM | 0.31 mL | 1.56 mL | 3.12 mL |
| 50 mM | 0.06 mL | 0.31 mL | 0.62 mL |
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Product Datasheets for API-2
References for API-2
References are publications that support the biological activity of the product.
Wotring et al (1990) Dual mechanisms of inhibition of DNA synthesis by triciribine. Cancer Res. 50 4891 PMID: 2379153
Ptak et al (1998) Phosphorylation of triciribine is necessary for activity against HIV type 1. AIDS Res.Hum.Retroviruses. 14 1315 PMID: 9788672
Yang et al (2004) Akt/protein kinase B signaling inhibitor-2, a selective small molecule inhibitor of Akt signaling with antitumour activity in cancer cells overexpressing Akt. Cancer Res. 64 4394 PMID: 15231645
If you know of a relevant reference for API-2, please let us know.
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Keywords: API-2, API-2 supplier, Selective, inhibitors, inhibits, Akt, PKB, signaling, Antitumor, antiviral, Protein, Kinase, B, NSC154020, Triciribine, NSC, 154020, TCN, (Protein, B), B/Akt, HIV, 2151, Tocris Bioscience
17 Citations for API-2
Citations are publications that use Tocris products. Selected citations for API-2 include:
Arqués et al (2016) Tankyrase Inhibition Blocks Wnt/β-Catenin Pathway and Reverts Resistance to PI3K and AKT Inhibitors in the Treatment of Colorectal Cancer. Clin Cancer Res 22 644 PMID: 26224873
Woo et al (2012) Calpain-mediated processing of p53-associated parkin-like cytoplasmic protein (PARC) affects chemosensitivity of human ovarian cancer cells by promoting p53 subcellular trafficking. J Biol Chem 287 3963 PMID: 22117079
Sunters et al (2010) Mechano-transduction in osteoblastic cells involves strain-regulated estrogen receptor alpha-mediated control of Ins-like growth factor (IGF) I receptor sensitivity to Ambient IGF, leading to phosphatidylinositol 3-kinase/AKT-dependent Wnt/LRP5 receptor-i J Biol Chem 285 8743 PMID: 20042609
Jackson et al (2010) Control of cerebellar long-term potentiation by P-Rex-family guanine-nucleotide exchange factors and phosphoinositide 3-kinase. PLoS One 5 e11962 PMID: 20694145
Liu et al (2010) FRP inhibits ox-LDL-induced endothelial cell apoptosis through an Akt-NF-{kappa}B-Bcl-2 pathway and inhibits endothelial cell apoptosis in an apoE-knockout mouse model. Am J Physiol Endocrinol Metab 299 E351 PMID: 20530739
Rosenberg et al (2015) Targeting Glutamatergic Signaling and the PI3 Kinase Pathway to Halt Melanoma Progression. Biol Open 8 42614 PMID: 25749171
Madhunapantula et al (2007) PRAS40 deregulates apoptosis in malignant melanoma. Cancer Res 67 3626 PMID: 17440074
Kuo et al (2014) Repression of glucocorticoid-stimulated angiopoietin-like 4 gene transcription by Ins. J Lipid Res 55 919 PMID: 24565756
Duan et al (2011) mTOR generates an auto-amplification loop by triggering the βTrCP- and CK1α-dependent degradation of DEPTOR. JAKSTAT 44 317 PMID: 22017877
Suarez et al (2017) The AKT inhibitor triciribine in combination with PTX has order-specific efficacy against Zfp217-induced breast cancer chemoresistance. Oncotarget 8 108534 PMID: 29312549
Ali et al (2017) Isolation and characterization of a new naturally immortalized human breast carcinoma cell line, KAIMRC1. BMC Cancer 17 803 PMID: 29187162
Robertson et al (2013) Sea urchin akt activity is Runx-dependent and required for post-cleavage stage cell division. Blood 2 472 PMID: 23789095
Yuan et al (2019) IFT80 is required for stem cell proliferation, differentiation, and odontoblast polarization during tooth development. Cell Death Dis 10 63 PMID: 30683845
Shravah et al (2014) PropF. mediates signal transducer and activator of transcription 3 activation and crosstalk with phosphoinositide 3-kinase/AKT. Am J Physiol Renal Physiol 3 e29554 PMID: 25105067
Barber and Sentman (2011) NKG2D receptor regulates human effector T-cell cytokine production. Mol Cell 117 6571 PMID: 21518928
Kana et al (2015) PI3K Phosphorylation Is Linked to Improved Electrical Excitability in an In Vitro Engineered Heart Tissue Disease Model System. Tissue Eng Part A 21 2379 PMID: 26120935
Roselli et al (2009) Disassembly of shank and homer synaptic clusters is driven by soluble beta-amyloid(1-40) through divergent NMDAR-dependent signalling pathways. PLoS One 4 e6011 PMID: 19547699
Do you know of a great paper that uses API-2 from Tocris? Please let us know.
Reviews for API-2
Average Rating: 5 (Based on 1 Review.)
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Attenuation by co-treatment of either PI3K inhibitor LY94002 or Akt inhibitor API-2.
By
Zhenmin Lei on 01/04/2018
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: Ovarian theca cells
The isolated mouse ovarian theca cells were maintained in 12-well plates withRPMI-1640 medium. For determination of Lhcgr expression, thecells were rinsed three times with PBS the day before incubation with vehicle(DMSO), 740YP (50 mg/ml), 740YP + API-2 (7.5 mM), LH (50 ng/mL),or LH + API-2 for 24 h. For determination of Akt phosphorylation,PBS rinsed cells were incubated with vehicle (DMSO), or API-2 (7.5 mM) in serum-free RPMI-medium for 1 h before the addition of LH (50 ng/mL) for 30 min.
Pathways for API-2
